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T62863 |
FLT3/ITD-IN-4
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FLT3/ITD-IN-4 (Compound 16) is a selective inhibitor of FLT3 internal tandem repeat mutations (FLT3-ITD) (IC50: 2.3 nM). FLT3/ITD-IN-4 can be used to study acute myeloid leukaemia. |
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T61415 |
FLT3/ITD-IN-1
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FLT3/ITD-IN-1 (Compound 1) is a highly potent inhibitor of FLT3 internal tandem duplications (FLT3-ITD). It exhibits remarkable inhibitory effects against FLT3 and FLT3-ITD, with impressive IC50 values of 38.2 nM and 144... |
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T62824 |
FLT3/ITD-IN-3
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FLT3/ITD-IN-3 (Compound 19) is a potent inhibitor of FLT3-ITD, acting on FLT3D835Y (IC50: 0.3 nM), FLT3 (IC50: 0.4 nM) and FLT3-ITD (IC50: 0.9 nM). FLT3/ITD-IN-3 showed potent inhibition of FLT3 phosphorylation and was e... |
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T63274 |
FLT3/ITD-IN-2
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FLT3/ITD-IN-2 is a potent inhibitor of FLT3-ITD and is able to act on FLT3D835Y (IC50: 0.3 nM), FLT3 (IC50: 0.4 nM) and FLT3-ITD (IC50: 1.0 nM).FLT3/ITD-IN-2 effectively inhibits the phosphorylation of FLT3 and is able t... |
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T2066 |
Quizartinib
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AC220 |
Apoptosis
,
FLT
,
Autophagy
,
Ligands for Target Protein for PROTAC
|
|
Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases. |
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T63629 |
PDGFRα/FLT3-ITD-IN-2
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PDGFRα/FLT3-ITD-IN-2 is a potent inhibitor of PDGFRα (IC50>20 μM) and FLT3 (IC50: 0.004 μM). PDGFRα/FLT3-ITD-IN-2 has shown investigational potential in acute myeloid leukemia or chronic eosinophilic leukemia. |
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T63454 |
PDGFRα/FLT3-ITD-IN-1
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PDGFRα/FLT3-ITD-IN-1 are potent inhibitors of PDGFRα/FLT3, and their IC50 values are greater than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 exhibits investigational potential in acute myeloid leukemia or chr... |
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T63127 |
PDGFRα/FLT3-ITD-IN-3
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PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα (IC50: 0.153 μM), FLT3 (IC50: 0.004 μM) and PDGFRα/FLT3-ITD-IN-3 has the potential to be studied in acute myeloid leukaemia or chronic eosinophilic leuk... |
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T1667 |
Tandutinib
|
MLN518,CT53518,NSC726292 |
Apoptosis
,
FLT
,
CSF-1R
,
PDGFR
,
Src
,
c-Kit
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Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versu... |
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T71857 |
GTP-14564
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FLT
,
Tyrosine Kinases
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GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba/F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentratio... |
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T9428 |
HM43239
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FLT
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HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the k... |
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T77763 |
Wu-5
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DUB
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Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis. |
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T27011 |
CHMFL-FLT3-122
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CHMFLFLT3122,CHMFL FLT3 122 |
FLT
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CHMFL-FLT3-122 is a potent and orally available FLT3 kinase inhibitor used to treat FLT3-ITD positive acute myeloid leukemia. CHMFL-FLT3-122 significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft m... |
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T1744 |
BIX02188
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Apoptosis
,
MEK
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BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD. |
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T4428 |
CCT241736
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FLT
,
Aurora Kinase
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CCT241736 is an orally bioavailable dual FLT3/Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinica... |
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T11300 |
FLT3-IN-6
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Others
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FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM. |
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T10622 |
BSc5371
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Others
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BSc5371 is a potent and irreversible FLT3 inhibitor (Kds: 1.3, 0.83, 1.5, 5.8, and 2.3 nM for mutant FLT3 D835H, FLT3 ITD/D835V, FLT3 ITD/F691L, FLT3-ITD, and wild type FLT3 wt). |
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T70597 |
G-749 hydrochloride
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G-749 hydrochloride is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. |
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T61329 |
HP1142
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HP1142 is a highly effective and specific inhibitor targeting the FLT3 receptor tyrosine kinase, with a particular affinity for its mutant variant FLT3/ITD. It exhibits a benzoimidazole scaffold-based structure, making i... |
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T77932 |
PF15 TFA
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PROTACs
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PF15 TFA, a PROTAC targeting FLT3 kinase and CRBN, exhibits selective degradation of FLT3-ITD with a DC50 of 76.7 nM. The compound potently suppresses proliferation in FLT3-ITD-positive cells, reduces phosphorylation lev... |
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T36681 |
Sorafenib N-oxide
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Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd =... |
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T2051 |
SKLB4771
|
FLT3-IN-1,FLT3-IN-1 |
FLT
|
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SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor. |
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T79490 |
LT-540-717
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LT-540-717 (compound 32), a potent FLT3 inhibitor (IC50=0.62 nM), exhibits antiproliferative activity and effectively inhibits various acquired FLT3 mutations, including FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y)... |
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T61758 |
HP1328
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HP1328 is a highly effective inhibitor of FLT3 receptor tyrosine kinase with a specific focus on FLT3/ITD mutation. It belongs to the benzoimidazole scaffold-based compound family. Significantly reducing the leukemia bur... |
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T81421 |
Pomalidomide-C5-Dovitinib
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PROTACs
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Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in FLT3-ITD+ acute myeloid leukemia (AML) cells. It promotes the... |
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T74259 |
PF15
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PROTACs
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PF15, a selective FLT3-ITD degrader, serves as a PROTAC (proteolysis targeting chimera) tethering ligands for FLT3 kinase and CRBN. It exhibits a degradation concentration 50 (DC50) of 76.7 nM and notably impedes the pro... |
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T63058 |
FLT3-IN-14
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FLT3-IN-14 is a potent inhibitor of FLT3, acting on FLT3-WT (IC50: 5.6 nM) and FLT3-ITD (IC50: 1.4 nM). FLT3-IN-14 inhibits FLT3 (Y591) phosphorylation, arrests the cell cycle in G1 phase and induces apoptosis. |
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T79596 |
FLT3-IN-20
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FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor, demonstrating IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD. It exhibits anti-proliferative effects on FLT3-ITD-positive AML cell lines, with IC50s of 7 nM... |
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T74707 |
PROTAC FLT3/CDK9 degrader-1
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PROTAC FLT3/CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1]. |
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T82392 |
FLT3-IN-23
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FLT3-IN-23 (compound 15), a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), exhibits an IC 50 value of 7.42 nM and demonstrates antiproliferative effects against BaF3 cells harboring diverse FLT3-TKD and FLT3-ITD-... |
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T81490 |
PHI-101
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PHI-101, an orally active FLT3 inhibitor, effectively overcomes resistance associated with numerous drug-resistant mutations. It potently suppresses both single activating FLT3 mutations (ITD or TKD mutants) and inhibits... |
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T62801 |
FLT3/TrKA-IN-1
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FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor, capable of acting on FLT3 (IC50: 43.8 nM), FLT3-ITD (IC50: 97.2 nM), FLT3-TKD (IC50: 92.5 nM) and TrKA (IC50: 23.6 nM). -FLT3/TrKA-IN-1 has potential for acute ... |
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T70779 |
BPR1J-340
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BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular prol... |
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T60794 |
HDAC10-IN-1
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HDAC10-IN-1 (compound 13b) is a potent and highly selective inhibitor of HDAC10 (IC 50 = 58 nM) that regulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells [1]. |
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T60760 |
HDAC10-IN-2
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HDAC10-IN-2 (compound 10c) regulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells. HDAC10-IN-2 is a potent and highly selective inhibitor of HDAC10 (IC50 = 20 nM) [1]. |
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T32288 |
JH-IX-179
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JH-IX179,JH-IX 179 |
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JH-IX-179 is a novel type I ATP competitive and highly selective FLT3 inhibitor. JH-IX-179 is much more selective for FLT3 and FLT3 mutants than for Kronani. In addition, JH-IX-179 showed little human serum protein bindi... |
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T78145 |
HDAC10-IN-2 hydrochloride
|
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Autophagy
|
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HDAC10-IN-2 hydrochloride (compound 10c) is an HDAC10 inhibitor with high potency and selectivity, exhibiting an IC50 of 20 nM. It influences autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells [1]. |
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T39085 |
SEL24-B489
|
SEL24-B489 |
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SEL24-B489 is a highly effective and orally bioavailable compound that acts as a robust, type I inhibitor of both PIM and FLT3-ITD. It exhibits exceptional binding affinity with K d values of 2 nM for PIM1, 2 nM for PIM2... |
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T79322 |
Antiproliferative agent-30
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Antiproliferative agent-30 (Compound 8g) demonstrates broad-spectrum antiproliferative activity, with IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM against HCT-116, K562, and MV-4-11 cancer cell lines, respectively. It... |
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T79391 |
FLT3-IN-21
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FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase. It effectively inhibits the proliferation of FLT3-ITD-positive AML cells MV-... |
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T68497 |
FI-700
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|
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FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibitio... |
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T35429 |
AC-4-130
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AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ul... |
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T70446 |
Abivertinib HCl
|
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|
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Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell p... |
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T68389 |
LY2457546
|
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LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 ... |
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T62417 |
MELK-8a
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MELK-8a (NVS-MELK8a) is a potent and selective inhibitor of maternal embryonic leucine elongation kinase (MELK) (IC50: 2 nM). 0.42 μM). Among them, MELK plays an important role in regulating mitosis in cancer cells. |
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T12555 |
PROTAC FLT-3 degrader 1
|
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Others
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PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity. |
